Abstract: Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Ar1 and Ar2 are independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; —X— is —N?CZ2—, —CY2?CZ2—, —CY2Y3—CHZ2—, —S—, —O—, or the like; Y1, Y2, Y3, Z1 and Z2 are independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Z1 and Z2 may be independently a linker group that may combine with Ar2 and Ar1 to form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate thereof; are disclosed.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Ar1 and Ar2 are independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; —X— is —N?CZ2—, —CY2?CZ2—, —CY2Y3—CHZ2—, —S—, —O—, or the like; Y1, Y2, Y3, Z1 and Z2 are independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Z1 and Z2 may be independently a linker group that may combine with Ar2 and Ar1 to form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate thereof; are disclosed.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Ar1 and Ar2 are independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; —X— is —N?CZ2-, —CY2?CZ2-, —CY2Y3—CHZ2-, —S—, —O—, or the like; Y1, Y2, Y3, Z1 and Z2 are independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Z1 and Z2 may be independently a linker group that may combine with Ar2 and Ar1 to form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate thereof; are disclosed.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.

Abstract: Pharmaceutical compositions for enhancing the expression of apoAI are provided.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided.

Abstract: Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments.

Abstract: Process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): ##STR1## is provided, said process comprising carrying out a stereoselective addition reaction of an o-(aminoalkylamino) thiophenyl derivative with a trans-substituted glycidic ester at an elevated temperature in a nonpolar solvent in the presence of a divalent or trivalent iron ion to prepare a threo-form intermediate, hydrolyzing the ester group of said intermediate, acetylating the hydroxyl group of said hydrolyzed compound, and subjecting said acetylated compound to a ring closure reaction to obtain the objective compound (VI).

Abstract: A compound of the formula: ##STR1## wherein X is .dbd.N--A--R.sup.1 or .dbd.C(R.sup.1)R.sup.2 ; A is a single bond, polymethylerie or --CO--; R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, unsubstituted or substituted phenyl, optionally substituted benzhydryl, or optionally substituted 5 to 6 membered heterocyclic group; Y is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-6 alkoxy, optionally substituted phenoxy, optionally substituted benzyloxy, or optionally substituted benzyl; Z is hydrogen or acyl; n is an integer of from 2 to 6, and pharmaceutically acceptable salt thereof. A pharmaceutical composition containing the compound, which is useful for treating hypertension and cardiac diseases, is also provided.

Abstract: A compound of the formula: ##STR1## wherein X is .dbd.N--A--R.sup.1 or .dbd.C(R.sup.1)R.sup.2 ; A is a single bond, polymethylene or --CO--; R.sup.1 and R.sup.2 are each hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, unsubstituted or substituted phenyl, optionally substituted benzhydryl, or optionally substituted 5 to 6 membered heterocyclic group; Y is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, optionally substituted phenoxy, optionally substituted benzyloxy, or optionally substituted benzyl; Z is hydrogen or acyl; n is an integer of from 2 to 6, and pharmaceutically acceptable salt thereof. A pharmaceutical composition containing the compound, which is useful for treating hypertension and cardiac diseases, is also provided.

Abstract: Novel Ca-blockers, 4,7-dihydropyrazolo[3,4-b]pyridine derivatives having potent antihypertensive and coronary vasodilating actions and useful in treatment for diseases in circulatory system, but without systole inhibitory action.

Abstract: 1,6-Dialkyl-3-substituted-4-nitrophenyl-4,7-dihydropyrazolo[3,4-b]pyridine- 5-carboxylic acid esters as Ca blocker having potent antihypertensive and coronary vasodilating actions and useful in treatment of diseases in circulatory system such as angina pectoris, hypertension, cerebrovascular dysfunction, arrhythmia, etc. with no systole inhibitory action, prepared from nitrobenzylideneacetoacetic acid esters on reaction with 3-substituted-5-amino-1-alkylpyrazoles.

Abstract: Lower alkyl 2-chloro-2-hydroxyiminoacetates are produced by (A) reacting chloral with a lower alkanol and a hydroxylamine salt in the presence of a Lewis acid or a metal oxide which is convertible into said Lewis acid during the course of the reaction to give a lower alkyl 2-hydroxyiminoacetate and then chlorinating the resulting product or (B) reacting chloral oxime with a lower alkanol in the presence of a base to give a lower alkyl 2-hydroxyiminoacetate and finally chlorinating the thus formed product.